P
US5059628AExpiredUtilityPatentIndex 56

Medical composition for percutaneous administration

Assignee: NITTO ELECTRIC IND COPriority: Sep 28, 1987Filed: Mar 14, 1990Granted: Oct 22, 1991
Est. expirySep 28, 2007(expired)· nominal 20-yr term from priority
Inventors:TSUDA YOKOSATOH SUSUMUOMATA TETSUO
A61K 47/183A61K 9/0014A61K 47/22
56
PatentIndex Score
3
Cited by
5
References
4
Claims

Abstract

A medical composition for external use comprising a proline ester represented by formula (I): ##STR1## wherein R 1 and R 2 are as defined in the specification, or a prolinol ester represented by formula (II): ##STR2## wherein R 3 and R 4 are as defined in the specification. The composition enhances percutaneous penetration absorption of an active ingredient to be combined therewith.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A method for enhancing percutaneous absorption of a pharmaceutically active compound comprising externally applying a medical composition to the skin of one in need thereof wherein said medical composition comprises: (a) a proline ester represented by formula (I): ##STR22## wherein R 1  represents a hydrogen atom or an aliphatic hydrocarbon residue, and R 2  represents an aliphatic hydrocarbon residue, with the total number of carbon atoms in R 1  and R 2  being 20 or less, or a prolinol ester represented by the formula (II): ##STR23## wherein R 3  represents a hydrogen atom or an aliphatic hydrocarbon residue, and R 4  represents an aliphatic hydrocarbon residue, with the total number of carbon atoms in R 3  and R 4  being 18 or less; and   (b) a pharmaceutically active compound.   
     
     
       2. A method as claimed in claim 1, wherein said medical composition further comprises at least one polar compound and said polar compound is at least one compound having nonpharmaceutical activity selected from the group consisting of lower mono alcohols having from 1 to 6 carbon atoms, glycerin, glycerin esters selected from the group consisting of mono-esters, diesters and triesters, thioglycerols, lactic esters having from 1 to 4 carbon atoms in the alcohol moiety, ethyleneurea derivatives thereof represented by formula (V): ##STR24## wherein R 5  and R 6  each represents a hydrogen atom or a lower alkyl group, amid compounds represented by formula (VI): ##STR25## wherein R 7 , R 8 , and R 9  each represents a hydrogen atom or a lower alkyl group, alkylene glycols, mono- or diethylene glycol monoalkyl esters, lactones, pyrrolidone compounds represented by formula (VII): ##STR26## wherein R 10  represents a hydrogen atom or a lower alkyl group, and lactam compounds represented by formula (VIII): ##STR27## wherein R 11  represents a lower alkyl group; and n represents 4 or 5. 
     
     
       3. A method as claimed in claim 2, wherein said polar compound is present in an amount of from 30 to 99.5% by weight based on the total weight of the proline ester or prolinol ester and the polar compound. 
     
     
       4. A method as claimed in claim 2, wherein said pharmaceutically active compound is present in an amount of from 0.01% to 20% by weight based on the total weight of the proline ester or prolinol ester and the polar compound.

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